5-Morpholinopyridin-3-amine → 5,7-difluoro-2-(5-fluoro-2-(methylsulfonyl)phenyl)-3-methyl-N-(5-morpholinopyridin-3-yl)quinolin-4-amine

Participants

Reaction Steps

Essentially prepared according to Procedure H using 4-chloro-5,7-difluoro-2-(5-fluoro-2-(methylsulfonyl)phenyl)-3-methylquinoline (120.0 mg, 0.32 mmol) and 5-morpholinopyridin-3-amine in toluene to give 5,7-difluoro-2-(5-fluoro-2-(methylsulfonyl)phenyl)-3-methyl-N-(5-morpholinopyridin-3-yl)quinolin-4-amine. 1H NMR (CDCl3) δ ppm 8.21 (1H, dd, J=8.8, 5.3 Hz), 7.93 (1H, d, J=2.3 Hz), 7.84 (1H, d, J=2.3 Hz), 7.49 (1H, ddd, J=9.2, 2.5, 1.4 Hz), 7.28-7.41 (2H, m), 7.14 (1H, dd, J=8.2, 2.5 Hz), 7.04-7.12 (1H, m), 6.55 (1H, t, J=2.4 Hz), 3.78 (4H, t, J=4.9 Hz), 3.11-3.24 (4H, m), 3.10 (3H, s), 1.91 (3H, s). Mass Spectrum (ESI) m/e=529.2 (M+1).

Provenance & Evidence